Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47819
Sirajis Salekin, T. Sharmin, Shahidur Rahman
Tolfenamic acid is a member of fenamate group of non-steroidal anti-inflammatory drugs (NSAID). It is generally used to treat migraine. In recent studies, metal complexes of traditional drugs like, manganese(II) complex of tolfenamic acid and mefenamic acid; cobalt(II) and zinc(II) complexes of tolfenamic acid are reported to give better biological activities than their parent drugs. In this study, tolfenamic acid was complexed with a divalent metal, cadmium(II) to form the drug-metal complex. The peripheral and central analgesic activities of this complex were tested to find out the impact of complexation on the pharmacological activity of the drug. Cadmium nitrate tetrahydrate was used for the complexation reaction and Fourier transform infrared (FT-IR) spectroscopic technique was used to identify the drug-metal complexation. Writhing method and tail flick technique were used to test peripheral and central analgesic activities, respectively in Swiss albino mice model. Comparison of the data obtained for positive and negative controls with the drug metal complex revealed a statistically significant increase in analgesic activities. Extensive experimentation is underway for further development in order to achieve better activity and assess toxicity profiles.
{"title":"Synthesis, Characterization and Analgesic Activity of Cadmium(II) Complex of Tolfenamic Acid","authors":"Sirajis Salekin, T. Sharmin, Shahidur Rahman","doi":"10.3329/dujps.v19i1.47819","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47819","url":null,"abstract":"Tolfenamic acid is a member of fenamate group of non-steroidal anti-inflammatory drugs (NSAID). It is generally used to treat migraine. In recent studies, metal complexes of traditional drugs like, manganese(II) complex of tolfenamic acid and mefenamic acid; cobalt(II) and zinc(II) complexes of tolfenamic acid are reported to give better biological activities than their parent drugs. In this study, tolfenamic acid was complexed with a divalent metal, cadmium(II) to form the drug-metal complex. The peripheral and central analgesic activities of this complex were tested to find out the impact of complexation on the pharmacological activity of the drug. Cadmium nitrate tetrahydrate was used for the complexation reaction and Fourier transform infrared (FT-IR) spectroscopic technique was used to identify the drug-metal complexation. Writhing method and tail flick technique were used to test peripheral and central analgesic activities, respectively in Swiss albino mice model. Comparison of the data obtained for positive and negative controls with the drug metal complex revealed a statistically significant increase in analgesic activities. Extensive experimentation is underway for further development in order to achieve better activity and assess toxicity profiles.","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73906323","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47823
Mohammad K. Islam, A. Barman, N. Qais
Now-a-days, cancer is a major concern globally, for which a large number of deaths occur annually, instead of the accessibility to various treatment options. Nevertheless, the latest treatment options are principally conglomerate with many side effects. Consequently, the development of an effective and competent anticancer therapy with the lower or minimum adverse or unwanted minor effect is the prime direction of research in the fields of natural product chemistry, drug design, and drug discovery. Phytochemicals available in plants have already been proven as prospective candidates in this regard. In general, phytochemicals are non-selective in their functions and restricted due to their differential activity on cancer cells along with the normal cells. As a consequence, researchers show their interest in isolating bioactive phytochemicals from nature with potent anticancer properties and generate lead compounds based on the natural skeleton of a molecule as a synthetic approach. Several phytomolecules have already been in existence for their in-vitro and in-vivo anticancer activities. This article deals with these lead phytomolecules from fifty-two species belong to thirty-five families with their reported mechanisms of action on nuclear and cellular factors involved in the treatment of carcinogenesis. Dhaka Univ. J. Pharm. Sci. 19(1): 83-96, 2020 (June)
{"title":"Anti-Cancer Constituents from Plants: Mini Review","authors":"Mohammad K. Islam, A. Barman, N. Qais","doi":"10.3329/dujps.v19i1.47823","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47823","url":null,"abstract":"Now-a-days, cancer is a major concern globally, for which a large number of deaths occur annually, instead of the accessibility to various treatment options. Nevertheless, the latest treatment options are principally conglomerate with many side effects. Consequently, the development of an effective and competent anticancer therapy with the lower or minimum adverse or unwanted minor effect is the prime direction of research in the fields of natural product chemistry, drug design, and drug discovery. Phytochemicals available in plants have already been proven as prospective candidates in this regard. In general, phytochemicals are non-selective in their functions and restricted due to their differential activity on cancer cells along with the normal cells. As a consequence, researchers show their interest in isolating bioactive phytochemicals from nature with potent anticancer properties and generate lead compounds based on the natural skeleton of a molecule as a synthetic approach. Several phytomolecules have already been in existence for their in-vitro and in-vivo anticancer activities. This article deals with these lead phytomolecules from fifty-two species belong to thirty-five families with their reported mechanisms of action on nuclear and cellular factors involved in the treatment of carcinogenesis. \u0000Dhaka Univ. J. Pharm. Sci. 19(1): 83-96, 2020 (June)","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88751012","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47812
Seagufta Afrin, Abdul Muhit, H. Sohrab, C. M. Hasan, M. Ahsan
The crude methanolic extract of the root bark of Pongamia pinnata was taken into consideration to isolate secondary metabolites. A total six known natural compounds were separated and purified by various chromatographic techniques and five isolates were identified as flavonoid derivatives such as pongachromene (1), kanugin (2), karanjin (3), demethoxykanugin (4), dimethoxypongapine (5) and the other is a triterpenoid (6). The pure compounds as well as petroleum ether, dichloromethane and ethyl acetate soluble fractions of crude methanolic extract were evaluated for bioactivities using established methods. In vitro antioxidant activity was studied by DPPH radical scavenging method using butylated hydroxyl anisole as standard. Among the pure compounds, kanugin and pongachromene showed significant antioxidant activity with the IC50 values of 27.20 ± 0.39 μg/mL and 43.53 ± 0.63 μg/ml, respectively as compared to the standard (23.87 ± 0.09 μg/ml), whereas karanjin, demethoxykanugin and dimethoxypongapine demonstrated moderate antioxidant activity. Mild thrombolytic activity was observed by different fractions with clot lysis ranging from 18.49 to 29.35% as compared to standard streptokinase (79.12%). The different solvent fractions and pure isolates showed very mild antimicrobial activity with zone of inhibition of 7.5 10.0 mm against the tested microorganisms using azithromycin and ketoconazole as standards. In the brine shrimp lethality bioassay, the dichloromethane, ethyl acetate, and methanol soluble fractions revealed significant lethality with LC50 values of 0.67 ± 0.05, 0.61 ± 0.13 and 0.56 ± 0.10 μg/ml, respectively as compared to standard tamoxifen (LC50 value 0.34 ± 0.09 μg/ml).
{"title":"Antioxidant, Thrombolytic, Antimicrobial and Cytotoxic Activities of Flavonoids Isolated from the Root Bark of Pongamia pinnata","authors":"Seagufta Afrin, Abdul Muhit, H. Sohrab, C. M. Hasan, M. Ahsan","doi":"10.3329/dujps.v19i1.47812","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47812","url":null,"abstract":"The crude methanolic extract of the root bark of Pongamia pinnata was taken into consideration to isolate secondary metabolites. A total six known natural compounds were separated and purified by various chromatographic techniques and five isolates were identified as flavonoid derivatives such as pongachromene (1), kanugin (2), karanjin (3), demethoxykanugin (4), dimethoxypongapine (5) and the other is a triterpenoid (6). The pure compounds as well as petroleum ether, dichloromethane and ethyl acetate soluble fractions of crude methanolic extract were evaluated for bioactivities using established methods. In vitro antioxidant activity was studied by DPPH radical scavenging method using butylated hydroxyl anisole as standard. Among the pure compounds, kanugin and pongachromene showed significant antioxidant activity with the IC50 values of 27.20 ± 0.39 μg/mL and 43.53 ± 0.63 μg/ml, respectively as compared to the standard (23.87 ± 0.09 μg/ml), whereas karanjin, demethoxykanugin and dimethoxypongapine demonstrated moderate antioxidant activity. Mild thrombolytic activity was observed by different fractions with clot lysis ranging from 18.49 to 29.35% as compared to standard streptokinase (79.12%). The different solvent fractions and pure isolates showed very mild antimicrobial activity with zone of inhibition of 7.5 10.0 mm against the tested microorganisms using azithromycin and ketoconazole as standards. In the brine shrimp lethality bioassay, the dichloromethane, ethyl acetate, and methanol soluble fractions revealed significant lethality with LC50 values of 0.67 ± 0.05, 0.61 ± 0.13 and 0.56 ± 0.10 μg/ml, respectively as compared to standard tamoxifen (LC50 value 0.34 ± 0.09 μg/ml).","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73966234","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47821
Shamweel Ahmad, Muslih A Alotaibi, Mohmmed S Alamri
Among gram-negative microorganisms Pseudomonas aeruginosa is the most common bacteria identified in different clinical specimens of hospitalized patients. A few studies have been conducted in Saudi Arabia regarding antibiotic susceptibility pattern. The purpose of this study was to evaluate the current levels of antibiotic susceptibility and to assess the resistance pattern of antibiotics among the clinical isolates of P. aeruginosa in the King Khalid Hospital, Alkharj, Kingdom of Saudi Arabia. This study was carried out during January, 2015 to May, 2015. A total of 180 different specimens such as sputum, urine, pus swabs, wound swabs etc. were collected from different patients admitted to the hospital. Thirty (30) clinical isolates of P. aeruginosa were isolated from different specimens of the patients suspected of having respiratory tract infection, urinary tract infection, wound infections, etc. The antibiotic susceptibility profiles of all the isolates were determined using Kirby-Bauer disk diffusion method. Piperacillin-tazobactam was found to be the most active antimicrobial agent with 96.7% susceptibility followed by cefepime (83.3%), ceftazidime (83.3%), and ciprofloxacin (76.7%). All isolates were resistant to ertapenem, cefuroxime, cefoxitin and nitrofurantoin. Anti-bacterial treatment strategies should focus on P. aeruginosa, for which the prevalence rates are increasing every year. The usage of piperacillin-tazobactam, cefepime, ceftazidime and ciprofloxacin must be reserved and only be given to the patients after susceptibility test to reduce the resistance of P. aeruginosa against these agents.
{"title":"Antibiotic Sensitivity Pattern of Clinical Isolates of Pseudomonas aeruginosa at a Tertiary Care Hospital in Saudi Arabia","authors":"Shamweel Ahmad, Muslih A Alotaibi, Mohmmed S Alamri","doi":"10.3329/dujps.v19i1.47821","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47821","url":null,"abstract":"Among gram-negative microorganisms Pseudomonas aeruginosa is the most common bacteria identified in different clinical specimens of hospitalized patients. A few studies have been conducted in Saudi Arabia regarding antibiotic susceptibility pattern. The purpose of this study was to evaluate the current levels of antibiotic susceptibility and to assess the resistance pattern of antibiotics among the clinical isolates of P. aeruginosa in the King Khalid Hospital, Alkharj, Kingdom of Saudi Arabia. This study was carried out during January, 2015 to May, 2015. A total of 180 different specimens such as sputum, urine, pus swabs, wound swabs etc. were collected from different patients admitted to the hospital. Thirty (30) clinical isolates of P. aeruginosa were isolated from different specimens of the patients suspected of having respiratory tract infection, urinary tract infection, wound infections, etc. The antibiotic susceptibility profiles of all the isolates were determined using Kirby-Bauer disk diffusion method. Piperacillin-tazobactam was found to be the most active antimicrobial agent with 96.7% susceptibility followed by cefepime (83.3%), ceftazidime (83.3%), and ciprofloxacin (76.7%). All isolates were resistant to ertapenem, cefuroxime, cefoxitin and nitrofurantoin. Anti-bacterial treatment strategies should focus on P. aeruginosa, for which the prevalence rates are increasing every year. The usage of piperacillin-tazobactam, cefepime, ceftazidime and ciprofloxacin must be reserved and only be given to the patients after susceptibility test to reduce the resistance of P. aeruginosa against these agents.","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91492115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47818
Sudipta Baroi, A. Saha, R. Bachar, S. C. Bachar
Inhibition of aromatase (CYTP450), a key enzyme in the estrogen biosynthesis, could result in regression of estrogen-dependent tumors and even prevent the promotion of breast cancer. The present research has been designed for searching a potent chemical moiety from natural sources to inhibit aromatase enzyme, the overfunctionality of which causes the breast cancer. Cannabis sativa contains a very much promising group of cannabinoids with more than 66 compounds with reported anticancer property and for the search of a target specific potent aromatase inhibitor, 61 cannabinoids from C. sativa were selected. The Structures Data File (SDF) of these ligand molecules were subjected to docking studies at the binding site of aromatase X-ray crystallographic structure based on lower resolution of the protein crystal structure and higher docking accuracy, predicted by calculating the correlation between experimental activities and Glide dock scores and compared with the standard aromatase ligand androstenedione and aromatase inhibitor fadrozole with existing drug for breast cancer treatment. The best docked pose of each ligand was selected on the basis of the highest dock score related to the binding free energies of the internal dataset compounds as compared to their observed activities. Apart from the hydrogen bond formation with the oxygen present on the aromatic ring system, the other parts of the molecules are stabilized by hydrophobic interactions with non-polar amino acid residues (Ile133, Phe134, Phe221, Trp224, Ile305, Ala306, Ala307, Val369, Val370, Leu372, Val373, Met374 and Leu477). From the screening results of the cannabinoid analogs, 21 out of 61 were found to have an acceptable docking score in comparison to the standards, androstenedione and fadrozole. The pharmacokinetic filters like absorption, distribution, metabolism and excretion and toxicity (ADMET) property determination were applied to select drug-like compounds. Among them three compounds were found to reveal the most promising drug like activity, which were cannabidiorcol (CN 17, CBD-C1), cannabitriol (CN 43, CBT) and cannabiripsol (CN 55, CBR). The ani-cancer activity of the target compounds was performed against brine shrimp lethality biassay, where cannabidiorcol exhibited significant LC50 value of 0.348 ±0.002 μg/ml (R2 = 0.9853) which is almost similar to vincristine sulfate (LC50 = 0.316±0.003 μg/ml, R2 = 0.9882). Compound cannabitriol also showed promisimg cytotoxicity 0.650±0.004 μg/ml (R2 = 0.9882) in comparison to the reference standard. But cannabiripsol demostrated relatively weaker activity 12.95±1.234 μg/ml (R2=0.9897). It can be concluded that the lead compounds may be developed as potent aromatase inhibitor performing their further biological evaluation.
{"title":"Cannabinoid as Potential Aromatase Inhibitor Through Molecular Modeling and Screening for Anti-Cancer Activity","authors":"Sudipta Baroi, A. Saha, R. Bachar, S. C. Bachar","doi":"10.3329/dujps.v19i1.47818","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47818","url":null,"abstract":"Inhibition of aromatase (CYTP450), a key enzyme in the estrogen biosynthesis, could result in regression of estrogen-dependent tumors and even prevent the promotion of breast cancer. The present research has been designed for searching a potent chemical moiety from natural sources to inhibit aromatase enzyme, the overfunctionality of which causes the breast cancer. Cannabis sativa contains a very much promising group of cannabinoids with more than 66 compounds with reported anticancer property and for the search of a target specific potent aromatase inhibitor, 61 cannabinoids from C. sativa were selected. The Structures Data File (SDF) of these ligand molecules were subjected to docking studies at the binding site of aromatase X-ray crystallographic structure based on lower resolution of the protein crystal structure and higher docking accuracy, predicted by calculating the correlation between experimental activities and Glide dock scores and compared with the standard aromatase ligand androstenedione and aromatase inhibitor fadrozole with existing drug for breast cancer treatment. The best docked pose of each ligand was selected on the basis of the highest dock score related to the binding free energies of the internal dataset compounds as compared to their observed activities. Apart from the hydrogen bond formation with the oxygen present on the aromatic ring system, the other parts of the molecules are stabilized by hydrophobic interactions with non-polar amino acid residues (Ile133, Phe134, Phe221, Trp224, Ile305, Ala306, Ala307, Val369, Val370, Leu372, Val373, Met374 and Leu477). From the screening results of the cannabinoid analogs, 21 out of 61 were found to have an acceptable docking score in comparison to the standards, androstenedione and fadrozole. The pharmacokinetic filters like absorption, distribution, metabolism and excretion and toxicity (ADMET) property determination were applied to select drug-like compounds. Among them three compounds were found to reveal the most promising drug like activity, which were cannabidiorcol (CN 17, CBD-C1), cannabitriol (CN 43, CBT) and cannabiripsol (CN 55, CBR). The ani-cancer activity of the target compounds was performed against brine shrimp lethality biassay, where cannabidiorcol exhibited significant LC50 value of 0.348 ±0.002 μg/ml (R2 = 0.9853) which is almost similar to vincristine sulfate (LC50 = 0.316±0.003 μg/ml, R2 = 0.9882). Compound cannabitriol also showed promisimg cytotoxicity 0.650±0.004 μg/ml (R2 = 0.9882) in comparison to the reference standard. But cannabiripsol demostrated relatively weaker activity 12.95±1.234 μg/ml (R2=0.9897). It can be concluded that the lead compounds may be developed as potent aromatase inhibitor performing their further biological evaluation.","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80824771","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47820
T. Saha, Nusrat Ahmed, Ikramul Hasan, Md. Selim Reza
In pharmaceutical industry, statistically valid experimental design can be utilized to optimize data in order to provide an economic and effective formulation, which could overcome several product and process development problems. Domperidone is a BCS Class II drug and has wide range of use, but has very poor bioavailability when administered orally because of degradation in intestinal fluid. The present study was focused on formulation, evaluation and optimization of mucoadhesive tablets of domperidone using a four-factor, three-level Box-Behnken design (BBD) so as to retain the prepared optimized formulation in gastric fluid for a prolong period of time in order to have better bioavailability and to get a sustained action. Physicochemical properties of the prepared formulations were determined according to the USP pharmacopeia official method and found satisfactory, except friability which was optimized to get the acceptable value. In-vitro dissolution study was performed for 8 hours for all the prepared formulations using USP II (paddle type) dissolution tester having 0.1N HCl (pH 1.2) as dissolution medium. Obtained data was further analyzed by means of quadratic response surface models so as to find out an optimize formulation in terms of desirable condition of dissolution rate after 1 hour, after 8 hours, total mucoadhesion time and tablet friability. Optimized formulation was further evaluated and it was found that, it was almost similar to the proposed optimized data. The formulation can provide a high degree of patient compliance, as sustained release formulation reduces the side effects and the cost of the formulation will be minimal as lesser amount of effort will be needed employing statistical model instead of conventional trial and error method.
{"title":"Preparation, Characterization and Optimization of Mucoadhesive Domperidone Tablets by Box Behnken Design","authors":"T. Saha, Nusrat Ahmed, Ikramul Hasan, Md. Selim Reza","doi":"10.3329/dujps.v19i1.47820","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47820","url":null,"abstract":"In pharmaceutical industry, statistically valid experimental design can be utilized to optimize data in order to provide an economic and effective formulation, which could overcome several product and process development problems. Domperidone is a BCS Class II drug and has wide range of use, but has very poor bioavailability when administered orally because of degradation in intestinal fluid. The present study was focused on formulation, evaluation and optimization of mucoadhesive tablets of domperidone using a four-factor, three-level Box-Behnken design (BBD) so as to retain the prepared optimized formulation in gastric fluid for a prolong period of time in order to have better bioavailability and to get a sustained action. Physicochemical properties of the prepared formulations were determined according to the USP pharmacopeia official method and found satisfactory, except friability which was optimized to get the acceptable value. In-vitro dissolution study was performed for 8 hours for all the prepared formulations using USP II (paddle type) dissolution tester having 0.1N HCl (pH 1.2) as dissolution medium. Obtained data was further analyzed by means of quadratic response surface models so as to find out an optimize formulation in terms of desirable condition of dissolution rate after 1 hour, after 8 hours, total mucoadhesion time and tablet friability. Optimized formulation was further evaluated and it was found that, it was almost similar to the proposed optimized data. The formulation can provide a high degree of patient compliance, as sustained release formulation reduces the side effects and the cost of the formulation will be minimal as lesser amount of effort will be needed employing statistical model instead of conventional trial and error method.","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83133278","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47813
Sakhawat Hossain, M. Rahaman, Atikur Rahman, J. Uddin, F. Ahmed
Methanolic extract of Curcuma amada leaves was investigated for isolation of secondary metabolites by successive chromatographic separation (VLC, column chromatography and TLC) which yielded several purified compounds. Among them the structures of β-sitosterol and stigmasterol were determined by analysis of high resolution H NMR spectroscopic data and co-TLC with authentic samples. The crude methanolic extract of C. amada leaves and its different fractionates i.e. petroleum ether (PESF), chloroform (CSF) and aqueous (AQSF) soluble fractions were evaluated for antibacterial, antioxidant, cytotoxic and thrombolytic activities. In antibacterial screening, the CSF exhibited the highest inhibition against bacterial growth having zone of inhibition 12 mm compared to the standard kanamycin where the zone of inhibition was observed at 18 mm against gram negative Vibrio mimicus. Significant free radical scavenging activity was also exhibited by CSF with the IC50 value of 103.09 μg/ml as compared to tert-butyl-1-hydroxytoluene (BHT) having IC50 31.88 μg/ml. In cytotoxicity study, the crude extract showed significant lethality towards brine shrimp having with the LC50 value of 6.540 μg/ml as compared to the standard vincristine sulfate (0.451μg/ml). In the study for thrombolytic property, different extracts of C. amada exhibited clot lysis ranging from 17.24 to 43.55% as compared to standard streptokinase (93.75 %).
{"title":"Phytochemical and Biological Investigation of Curcuma amada Leaves","authors":"Sakhawat Hossain, M. Rahaman, Atikur Rahman, J. Uddin, F. Ahmed","doi":"10.3329/dujps.v19i1.47813","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47813","url":null,"abstract":"Methanolic extract of Curcuma amada leaves was investigated for isolation of secondary metabolites by successive chromatographic separation (VLC, column chromatography and TLC) which yielded several purified compounds. Among them the structures of β-sitosterol and stigmasterol were determined by analysis of high resolution H NMR spectroscopic data and co-TLC with authentic samples. The crude methanolic extract of C. amada leaves and its different fractionates i.e. petroleum ether (PESF), chloroform (CSF) and aqueous (AQSF) soluble fractions were evaluated for antibacterial, antioxidant, cytotoxic and thrombolytic activities. In antibacterial screening, the CSF exhibited the highest inhibition against bacterial growth having zone of inhibition 12 mm compared to the standard kanamycin where the zone of inhibition was observed at 18 mm against gram negative Vibrio mimicus. Significant free radical scavenging activity was also exhibited by CSF with the IC50 value of 103.09 μg/ml as compared to tert-butyl-1-hydroxytoluene (BHT) having IC50 31.88 μg/ml. In cytotoxicity study, the crude extract showed significant lethality towards brine shrimp having with the LC50 value of 6.540 μg/ml as compared to the standard vincristine sulfate (0.451μg/ml). In the study for thrombolytic property, different extracts of C. amada exhibited clot lysis ranging from 17.24 to 43.55% as compared to standard streptokinase (93.75 %).","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74760412","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47817
Shejuti Rahman Brishty, Poushali Saha, Z. A. Mahmud, S. Rahman
The present study describes the synthesis and pharmacological evaluation of a number of substituted benzimidazole derivatives designated by 3A-1, 3A-2, 3A-3, 3B-1 and 3B-2 through condensation of different o-aryldiamine compounds with the corresponding aldehyde employing ammonium salt as a catalyst. All the compounds were characterized by IR and H NMR spectroscopic analysis. The synthesized benzimidazole derivatives were investigated for analgesic and antioxidant activities using acetic acid-induced writhing inhibition in Swiss albino mice and DPPH free radical scavenging assay, respectively. Compounds 3A-3, 3B-1 and 3B-2 at a dose of 50 mg/kg body weight reduced the number of writhings by 88.24%, 84.03% and 85.71%, respectively (p<0.001) in comparison with standard diclofenac (90.76% inhibition). The derivatives 3A-1, 3A-2, 3A-3 and 3B-2 showed prominent antioxidant activity with IC50 values of 0.038, 0.959, 8.834 and 7.519 μg/ml, respectively in comparison with the standard butylated hydroxytoluene (BHT) (14.44 μg/ml). Among the synthesized compounds, 3A-3 and 3B2 emerged as the most promising analgesic and antioxidant agents and expressed their potential as lead compounds in future research.
{"title":"Synthesis and Evaluation of Analgesic and Antioxidant Activities of Substituted Benzimidazole Derivatives","authors":"Shejuti Rahman Brishty, Poushali Saha, Z. A. Mahmud, S. Rahman","doi":"10.3329/dujps.v19i1.47817","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47817","url":null,"abstract":"The present study describes the synthesis and pharmacological evaluation of a number of substituted benzimidazole derivatives designated by 3A-1, 3A-2, 3A-3, 3B-1 and 3B-2 through condensation of different o-aryldiamine compounds with the corresponding aldehyde employing ammonium salt as a catalyst. All the compounds were characterized by IR and H NMR spectroscopic analysis. The synthesized benzimidazole derivatives were investigated for analgesic and antioxidant activities using acetic acid-induced writhing inhibition in Swiss albino mice and DPPH free radical scavenging assay, respectively. Compounds 3A-3, 3B-1 and 3B-2 at a dose of 50 mg/kg body weight reduced the number of writhings by 88.24%, 84.03% and 85.71%, respectively (p<0.001) in comparison with standard diclofenac (90.76% inhibition). The derivatives 3A-1, 3A-2, 3A-3 and 3B-2 showed prominent antioxidant activity with IC50 values of 0.038, 0.959, 8.834 and 7.519 μg/ml, respectively in comparison with the standard butylated hydroxytoluene (BHT) (14.44 μg/ml). Among the synthesized compounds, 3A-3 and 3B2 emerged as the most promising analgesic and antioxidant agents and expressed their potential as lead compounds in future research.","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89678198","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47816
C. Nnadi, Ndidiamaka H. Okorie, Mbah Cj
The study was designed to develop and characterize structured vehicles for effective delivery of glipizide (GPZ) through excised stratum corneum (SC). Several mixed binary systems of ethanol or propylene glycol (PG) were prepared by homogeneous mixing with double distilled water. Different microemulsions were prepared by titration method and their physicochemical properties determined. Transdermal permeation of GPZ was studied in-vitro using modified Franz diffusion cells. Apart from the slight difference in their pH values, there was no significant difference in the physicochemical properties of the drug-loaded coconut oil-based microemulsions and their blank counterparts. Transdermal flux was highest in binary mixtures of 9:1 (v/v) aqueous ethanol (Jss 30.25 ± 5.75 μg/cmh) and PG (Jss 6.34 ± 1.29 μg/cmh) compared to their lower strengths. Transdermal GPZ flux, Jss, μg/cmh was higher in o/w (121.2 ± 9.98) compared to w/o (3.89 ± 0.19) microemulsions with enhanced permeation of ≥ 23 fold using patch size of 10.45 cm. Biophysical analysis of untreated and treated SC showed that GPZ permeation could depend on the extent of disruption of lipid and protein bilayers of SC by the vehicles. Cremophor RH 40/ethanol/coconut oil-based o/w microemulsion and 9:1 v/v mixed binary systems of ethanol or PG are promising vehicles for delivery of GPZ transdermally.
{"title":"Disruption of Lipid Bilayers of Stratum Corneum by Transdermal Delivery of Glipizide in Microemulsion and Binary Co-solvent Systems","authors":"C. Nnadi, Ndidiamaka H. Okorie, Mbah Cj","doi":"10.3329/dujps.v19i1.47816","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47816","url":null,"abstract":"The study was designed to develop and characterize structured vehicles for effective delivery of glipizide (GPZ) through excised stratum corneum (SC). Several mixed binary systems of ethanol or propylene glycol (PG) were prepared by homogeneous mixing with double distilled water. Different microemulsions were prepared by titration method and their physicochemical properties determined. Transdermal permeation of GPZ was studied in-vitro using modified Franz diffusion cells. Apart from the slight difference in their pH values, there was no significant difference in the physicochemical properties of the drug-loaded coconut oil-based microemulsions and their blank counterparts. Transdermal flux was highest in binary mixtures of 9:1 (v/v) aqueous ethanol (Jss 30.25 ± 5.75 μg/cmh) and PG (Jss 6.34 ± 1.29 μg/cmh) compared to their lower strengths. Transdermal GPZ flux, Jss, μg/cmh was higher in o/w (121.2 ± 9.98) compared to w/o (3.89 ± 0.19) microemulsions with enhanced permeation of ≥ 23 fold using patch size of 10.45 cm. Biophysical analysis of untreated and treated SC showed that GPZ permeation could depend on the extent of disruption of lipid and protein bilayers of SC by the vehicles. Cremophor RH 40/ethanol/coconut oil-based o/w microemulsion and 9:1 v/v mixed binary systems of ethanol or PG are promising vehicles for delivery of GPZ transdermally.","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87548150","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-26DOI: 10.3329/dujps.v19i1.47815
Suciati, Lusiana Arifianti
Marine sponges have been known as the source of natural products. Various metabolites with potent bioactivities have been reported from this organism. The current study aims to investigate the anticancer potency of three marine sponges namely Diacarnus debeauforti, Haliclona amboinensis and Agelas cavernosa collected from Barrang Lompo Island, South Sulawesi, Indonesia. The ethyl acetate extracts of the sponges were screened against T47D breast cancer cells and HeLa cervical cancer cells by using the MTT method. The results showed that these sponges demonstrated anticancer activity against both cancer cell lines. The lowest IC50 of 18.2 μg/ml was given by the extract of A. cavernosa against T47D cell line, while in the screening against HeLa cancer cell line, the extract of D. debeauforti revealed the highest potency with IC50 of 15.7 μg/ml. Our results suggested that the marine sponges namely D. debeauforti, H. amboinensis and A. cavernosa can be good candidates for the development of anticancer agents.
{"title":"In vitro Anticancer Activity of Marine Sponges Against T47D and HeLa Cell Lines","authors":"Suciati, Lusiana Arifianti","doi":"10.3329/dujps.v19i1.47815","DOIUrl":"https://doi.org/10.3329/dujps.v19i1.47815","url":null,"abstract":"Marine sponges have been known as the source of natural products. Various metabolites with potent bioactivities have been reported from this organism. The current study aims to investigate the anticancer potency of three marine sponges namely Diacarnus debeauforti, Haliclona amboinensis and Agelas cavernosa collected from Barrang Lompo Island, South Sulawesi, Indonesia. The ethyl acetate extracts of the sponges were screened against T47D breast cancer cells and HeLa cervical cancer cells by using the MTT method. The results showed that these sponges demonstrated anticancer activity against both cancer cell lines. The lowest IC50 of 18.2 μg/ml was given by the extract of A. cavernosa against T47D cell line, while in the screening against HeLa cancer cell line, the extract of D. debeauforti revealed the highest potency with IC50 of 15.7 μg/ml. Our results suggested that the marine sponges namely D. debeauforti, H. amboinensis and A. cavernosa can be good candidates for the development of anticancer agents.","PeriodicalId":11304,"journal":{"name":"Dhaka University Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87609608","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：